Assay Detail
Binding
CHEMBL4844392
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Protac activity at VHL/AR T878A mutant in human LNCaP cells assessed as induction of AR degradation measured after 24 hrs by western blot analysis
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
von Hippel-Lindau disease tumor suppressor/Androgen receptor (CHEMBL4523730) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.51 | 8.85 |
| EC90 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861919 | — | — | 2 | 8.85 |
| CHEMBL4879244 | — | — | 2 | 8.85 |
| CHEMBL4867584 | — | — | 2 | 8.47 |
| CHEMBL4747369 | — | — | 2 | 8.29 |
| CHEMBL4877348 | — | — | 2 | 8.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861919 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4879244 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4867584 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4747369 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4877348 | — | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4747369 | — | EC90 | = | 41.0 | nM | - |
| CHEMBL4861919 | — | EC90 | = | 52.0 | nM | - |
| CHEMBL4877348 | — | EC90 | = | 25.0 | nM | - |
| CHEMBL4879244 | — | EC90 | = | 10.0 | nM | - |
| CHEMBL4867584 | — | EC90 | = | 10.0 | nM | - |